Melanin Concentrating Hormone Receptor Antagonists as Antiobesity Agents: From M2 to MCHR-1

Title: Melanin Concentrating Hormone Receptor Antagonists as Antiobesity Agents: From M2 to MCHR-1

Volume: 7 Issue: 15

Author(s): Mark D. McBriar

Affiliation:

Keywords: Melanin-concentrating hormone, MCH, MCH R1, MCH R1 antagonist, obesity

Abstract: Melanin concentrating hormone (MCH) is a cyclic, nonadecapeptide expressed in the CNS of all vertebrates that regulates feeding behavior and energy homeostasis. The MCH-1 receptor (MCH-R1) has been identified as a key target in MCH regulation, as small molecule antagonists of MCH-R1 have demonstrated activity in vivo. Herein, we chronicle our efforts to optimize a hit identified via high throughput screening of our proprietary compound library. Several challenges such as selectivity over other receptors, toxicity of a potential metabolite and determining receptor occupancy via a medium throughput assay will be reviewed.

Cite this article as:

McBriar D. Mark, Melanin Concentrating Hormone Receptor Antagonists as Antiobesity Agents: From M2 to MCHR-1, Current Topics in Medicinal Chemistry 2007; 7 (15) . https://dx.doi.org/10.2174/156802607782194752